The advantages of controlled release products are well known in the pharmaceutical field and include the ability to maintain a desired blood level of a medicament over a comparatively longer period of time while increasing patient compliance by reducing the number of administrations necessary to achieve the same. These advantages have been attained by a wide variety of methods. For example, different hydrogels have been described for use in controlled release medicines, some of which are synthetic, but most of which are semi-synthetic or of natural origin. A few contain both synthetic and non-synthetic material. However, some of the systems require special process and production equipment, and in addition some of these systems are susceptible to variable drug release.
Oral controlled release delivery systems should ideally be adaptable so that release rates and profiles can be matched to physiological and chronotherapeutic requirements.
While many controlled and sustained release formulations are already known for a variety of pharmaceutically active agents, to date there have not been any commercially available controlled or sustained release formulations for the drug oxybutynin, which is an antispasmodic agent for treating neurogenic bladders in humans.
In the United States, oxybutynin is commercially available as the chloride salt as Ditropan.RTM. (Marion Merrell Dow Inc.) in both a 5 milligram tablet and as a syrup (5 mg/5 ml), and is also available as Urotrol.RTM. (Baker Norton Pharmaceuticals, Inc.) as a 5 milligram tablet. Those formulations are said to provide an onset of effect 30-60 minutes after oral administration, a peak effect 3-6 hours after administration, and a duration of effect ranging from 6-10 hours. The formulation is usually administered to adults two-three times daily. The maximum dosage is considered to be 5 mg administered four times daily.
Previously, a heterodisperse polysaccharide excipient system and controlled release oral solid dosage forms were described in our U.S. Pat. Nos. 4,994,276, 5,128,143, and 5,135,757. These systems are commercially available under the tradename TIMERx.TM. from Edward Mendell Co., Inc., Patterson, N.Y., which is the assignee of the present invention. These patents are hereby incorporated by reference.